Surface charged temoporfin-loaded flexible vesicles: In vitro skin penetration studies and stability
Surface charged temoporfin-loaded flexible vesicles: In vitro skin penetration studies and stability
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DOI：
10.1016/j.ijpharm.2009.10.006
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发表时间：
2010-01-15
影响因子：
5.8
通讯作者：
Fahr, Alfred
中科院分区：
文献类型：
--
作者：
Dragicevic-Curic, Nina;Graefe, Susanna;Fahr, Alfred
为了提高替普芬(MTHPC)的局部给药效率，制备了一种低透皮吸收的高疏水性光敏剂中性、阴离子和阳离子柔性脂质体(即柔脂体)，并对其促透性能进行了考察。体外皮肤渗透研究是使用安装在Franz扩散池中的人腹部皮肤。考察了柔软体表面电荷对mTHPC透皮性能的影响，以及对囊泡的物理性质(粒径、多分散性指数、片层性)和理化稳定性的影响。光子相关光谱表明，制备后的囊泡具有较小的颗粒尺寸和较低的多分散性指数，而冷冻电子显微镜证实这些囊泡大多为单层球形。在稳定性方面，与缺乏长期稳定性的阴离子柔体相比，中性和阳离子柔体在4℃下保存9个月都是稳定的。在渗透促进能力方面，阳离子柔体具有最高的穿透能力，即与传统脂质体、中性和阴离子柔体相比，阳离子柔体向角质层和皮肤深层输送mTHPC的量最高。综上所述，mTHPC阳离子柔体有望成为一种将mTHPC输送到皮肤的工具，这将有利于皮肤恶性或非恶性疾病的光动力学治疗。(C)2009爱思唯尔B.V.保留所有权利。
In order to increase topical delivery of temoporfin (mTHPC), a highly hydrophobic photosensitizer with low percutaneous penetration, neutral, anionic and cationic flexible liposomes (i.e. flexosomes) were prepared and investigated for their penetration enhancing ability. The in vitro skin penetration study was performed using human abdominal skin mounted in Franz diffusion cells. Besides the effect of surface charge of flexosomes on skin penetration of mTHPC, also its effect on physical properties (particle size, polydispersity index, lamellarity) and physicochemical stability of vesicles was investigated. Photon-correlation spectroscopy revealed that vesicles had after preparation a small particle size and low polydispersity index, while cryo-electron microscopy confirmed that these vesicles were mostly unilamellar and of a spherical shape. Regarding stability, contrasting to anionic flexosomes showing lack of long-term stability, neutral and cationic flexosomes were stable during 9 months storage at 4 degrees C. As to the penetration enhancing ability, cationic flexosomes possessed the highest, i.e. they delivered the highest mTHPC-amount to stratum corneum and deeper skin layers compared to conventional liposomes, neutral and anionic flexosomes.In conclusion, mTHPC-loaded cationic flexosomes could be a promising tool for delivering mTHPC to the skin, which would be beneficial for the photodynamic therapy of cutaneous malignant or non-malignant diseases. (C) 2009 Elsevier B.V. All rights reserved.